组胺和抗组胺药的研究进展  

Update on histamine and antihistamines

作　　者：吴银华[1] 方红[1] 

机构地区：[1]浙江大学医学院附属第一医院皮肤科,杭州310003

出　　处：《国际皮肤性病学杂志》2013年第6期358-361,共4页International Journal of Dermatology and Venereology

基　　金：2011年度中华医学会皮肤性病学分会万马药业皮肤病学研究基金

摘　　要：组胺与H1受体结合可增强抗原提呈细胞的能力，促进肥大细胞和嗜碱性粒细胞中组胺和其他介质的释放，在荨麻疹等过敏性疾病的发病中起着作用。第一代川抗组胺药由于相对分子质量小，嗜脂性，易通过血脑屏障，临床应用可产生较多不良反应，尤其是对警觉性、认知等的影响。第二代H1抗组胺药相对分子质量大，受体专一性强、亲和力高，抗组胺活性更强，安全性更好，国外指南均推荐作为荨麻疹的一线治疗药物，治疗剂量可增至标准剂量的4倍以提高疗效，仍具有很好的安全性。H3、H4抗组胺药也已进入临床试验，有望治疗过敏性疾病及瘙痒症。The binding of histamine to H1 receptors may result in an increase in the capacity of antigen-presenting cells and in the release of histamine and other mediators from mast ceils and basophils, which plays an important role in the pathogenesis of urticaria and other allergic diseases. First-generation H1- antihistamines, which have lipophilicity and low molecular weight, can penetrate blood-brain barrier easily and induce a number of side effects, especially on alertness and consciousness. By contrast, second-generation H1- antihistamines have higher molecular weight, specificity and affinity for receptor, stronger antihistamine activity, and superior safety. International treatment guidelines all recommend second-generation H1- antihistamines as first-choice therapy for chronic urticaria, which permits a dose increase up to 4 times the standard dose when needed with a good security. H3- and H4- antihistamines are under clinical investigations, and are expected to be used for the treatment of allergic diseases and pruritus.

关 键 词：荨麻疹 组胺 组胺H1拮抗剂 

分 类 号：R976[医药卫生—药品]